MSAB是Wnt/β-catenin信号传导的有效和选择性抑制剂。MSAB与β-catenin结合，促进其降解，并特别下调Wnt/β-catenin靶基因。MSAB对Wnt依赖性癌细胞显示出有效的抗肿瘤作用。
货号:ajcx31120
CAS:173436-66-3
分子式:C15H15NO4S
分子量：305.35
溶解度:DMSO: 250 mg/mL (818.73 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

MSAB is a potent and selective inhibitor of Wnt/β-catenin signaling. MSAB binds to β-catenin promoting its degradation, and specifically downregulates Wnt/β-catenin target genes. MSAB exhibits potent anti-tumor effects selectively on Wnt-dependent cancer cells[1].

MSAB (2-10 μM) selectively decreases cell viability of Wnt-dependent cells while showing little effect on Wnt-independent cells and normal human cells[1].MSAB (0.01-10 μM; 20 h) inhibits T-cell factor (TCF) luciferase reporter activity in HCT116 cells[1].MSAB (20 h) suppresses the Wnt3a-induced TOP-Luc activation and increases of active β-catenin levels in HEK293T cells[1].MSAB (0.5-10 μM; 20 h) decreases mRNA and protein levels of endogenous Wnt target genes in HCT116 cells[1].MSAB (5 μM; 16 h) induces degradation of β-catenin in a proteasome-dependent manner in HCT116 cells[1].

MSAB (10-20 mg/kg; i.p. daily for 2 weeks) inhibits tumor growth of Wnt-dependent cancer cells in mouse xenograft model[1].MSAB (10-20 mg/kg; i.p. twice daily for 2 weeks) inhibits tumor growth of MMTV-Wnt1 transgenic mice[1]. Animal Model: Athymic nude mice (5-6 weeks) are injected HCT116, HT115, H23, or H460 cells[1]

[1]. Hwang SY, et, al. Direct Targeting of β-Catenin by a Small Molecule Stimulates Proteasomal Degradation and Suppresses Oncogenic Wnt/β-Catenin Signaling. Cell Rep. 2016 Jun 28;16(1):28-36.